Advances in the fields of chemical genetics and molecular cell biology have led to the development of genetic manipulation-based therapies for cancer. Gabhann et al. (2010) Curr. Opin. Mol. Ther. 12:570-577. Such genetic manipulation methods typically rely on either the small-molecule/protein modalities (Collins et al. (2006) Nat. Chem. Biol. 2:689-700) or RNA interference (RNAi)-based modalities (Kim et al. (2007) Nat. Rev. Gen. 8:173-184), each having their own advantages and disadvantages. For example, RNAi therapeutics can provide attractive solutions to the major shortcomings of the conventional therapeutics, including difficulty in lead identification and complex synthesis of small organic molecules and proteins, and potentially can be applicable to all molecular targets for cancer therapy. Bumcrot et al. (2006) Nat. Chem. Biol. 2:711-719. However, RNAi-based therapeutics, such as small interfering RNA (siRNA) and micro RNA (miRNA), are inherently antagonistic and their downstream effects (i.e. gene-silencing) are delayed, compared to those of conventional small-molecule/protein-based therapeutics. Castanotto et al. (2009) Nature 457:426-433. Additionally, owing to their short serum half-life and poor cellular uptake, successful clinical application of siRNA requires appropriate chemical modifications and better delivery vehicles to overcome the numerous cellular barriers. Kim et al. On the other hand, small organic molecules can act as both antagonists and agonists for molecular targets and their drug effects can be much faster than siRNA with minimal problems during their intracellular uptake. Bumcrot et al. The present invention addresses the deficiencies of current genetic manipulation-based therapies.